alleen voor onderzoeksdoeleinden
PF-4708671 S6 Kinase remmer
Cat.nr.S2163
Chemische structuur
Molecuulgewicht: 390.41
Kwaliteitscontrole
| Gerelateerde doelwitten | PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A |
|---|---|
| Overig S6 Kinase Inhibitoren | BI-D1870 LY2584702 LY2584702 Tosylate LJH685 LJI308 S6K-18 3'-Hydroxypterostilbene L-Norvaline BRD7389 Gingerenone A |
Celkweek, behandeling & werkzame concentratie
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | ||||
| UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | ||||
| A427 | Growth Inhibition Assay | IC50=5.72567 μM | ||||
| OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | ||||
| SW684 | Growth Inhibition Assay | IC50=7.52268 μM | ||||
| SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | ||||
| CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | ||||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | ||||
| ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | ||||
| OE19 | Growth Inhibition Assay | IC50=10.1733 μM | ||||
| DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | ||||
| SW13 | Growth Inhibition Assay | IC50=11.9319 μM | ||||
| MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | ||||
| 647-V | Growth Inhibition Assay | IC50=12.3582 μM | ||||
| NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | ||||
| LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | ||||
| UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | ||||
| NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | ||||
| FADU | Growth Inhibition Assay | IC50=13.6992 μM | ||||
| A2780 | Growth Inhibition Assay | IC50=13.8041 μM | ||||
| NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | ||||
| TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | ||||
| HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | ||||
| MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | ||||
| Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | ||||
| HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | ||||
| SAS | Growth Inhibition Assay | IC50=18.6455 μM | ||||
| IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | ||||
| C3A | Growth Inhibition Assay | IC50=18.7919 μM | ||||
| ES3 | Growth Inhibition Assay | IC50=18.8364 μM | ||||
| HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | ||||
| T47D | Growth Inhibition Assay | IC50=20.1485 μM | ||||
| EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | ||||
| LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | ||||
| U031 | Growth Inhibition Assay | IC50=21.4802 μM | ||||
| A549 | Growth Inhibition Assay | IC50=21.8491 μM | ||||
| RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | ||||
| BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | ||||
| NB69 | Growth Inhibition Assay | IC50=23.152 μM | ||||
| NB7 | Growth Inhibition Assay | IC50=24.188 μM | ||||
| HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | ||||
| MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | ||||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | ||||
| HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | ||||
| Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | ||||
| KGN | Growth Inhibition Assay | IC50=25.7547 μM | ||||
| LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | ||||
| NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | ||||
| D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | ||||
| DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | ||||
| NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | ||||
| KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | ||||
| C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | ||||
| SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | ||||
| MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | ||||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | ||||
| CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | ||||
| GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | ||||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | ||||
| KLE | Growth Inhibition Assay | IC50=33.4334 μM | ||||
| KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | ||||
| DOK | Growth Inhibition Assay | IC50=34.6612 μM | ||||
| ACHN | Growth Inhibition Assay | IC50=35.1588 μM | ||||
| KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | ||||
| SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | ||||
| NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | ||||
| ES7 | Growth Inhibition Assay | IC50=36.2249 μM | ||||
| A172 | Growth Inhibition Assay | IC50=36.4187 μM | ||||
| UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | ||||
| LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | ||||
| KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | ||||
| TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | ||||
| G-402 | Growth Inhibition Assay | IC50=40.061 μM | ||||
| 786-0 | Growth Inhibition Assay | IC50=40.9096 μM | ||||
| K5 | Growth Inhibition Assay | IC50=41.3686 μM | ||||
| SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | ||||
| OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | ||||
| T84 | Growth Inhibition Assay | IC50=42.1263 μM | ||||
| GCIY | Growth Inhibition Assay | IC50=43.0803 μM | ||||
| BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | ||||
| SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | ||||
| TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | ||||
| 23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | ||||
| DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | ||||
| ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | ||||
| DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | ||||
| COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | ||||
| DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | ||||
| YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | ||||
| RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | ||||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | ||||
| NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | ||||
| OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | ||||
| NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | ||||
| 22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | ||||
| G-401 | Growth Inhibition Assay | IC50=48.4415 μM | ||||
| YAPC | Growth Inhibition Assay | IC50=49.8073 μM | ||||
| SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | ||||
| COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | ||||
| KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | ||||
| NB5 | Growth Inhibition Assay | IC50=51.4509 μM | ||||
| CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | ||||
| CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | ||||
| CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | ||||
| 8305C | Growth Inhibition Assay | IC50=52.315 μM | ||||
| Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | ||||
| AU565 | Growth Inhibition Assay | IC50=52.5509 μM | ||||
| CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | ||||
| BEN | Growth Inhibition Assay | IC50=53.7862 μM | ||||
| NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | ||||
| HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | ||||
| SH-4 | Growth Inhibition Assay | IC50=54.138 μM | ||||
| NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | ||||
| BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | ||||
| CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | ||||
| A388 | Growth Inhibition Assay | IC50=56.0985 μM | ||||
| C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | ||||
| GAMG | Growth Inhibition Assay | IC50=56.5955 μM | ||||
| MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | ||||
| VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | ||||
| HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | ||||
| BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | ||||
| LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | ||||
| LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | ||||
| NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | ||||
| COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | ||||
| OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | ||||
| SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | ||||
| MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | ||||
| SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | ||||
| EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | ||||
| GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | ||||
| HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | ||||
| MLMA | Growth Inhibition Assay | IC50=61.6163 μM | ||||
| D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | ||||
| SF295 | Growth Inhibition Assay | IC50=63.6655 μM | ||||
| ES4 | Growth Inhibition Assay | IC50=64.4719 μM | ||||
| CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | ||||
| OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | ||||
| NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | ||||
| JAR | Growth Inhibition Assay | IC50=65.5516 μM | ||||
| SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | ||||
| D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | ||||
| EW-22 | Growth Inhibition Assay | IC50=66.395 μM | ||||
| GCT | Growth Inhibition Assay | IC50=67.0443 μM | ||||
| NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | ||||
| RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | ||||
| HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | ||||
| NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | ||||
| IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | ||||
| SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | ||||
| SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | ||||
| LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | ||||
| U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | ||||
| KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | ||||
| U251 | Growth Inhibition Assay | IC50=73.8168 μM | ||||
| HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | ||||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | ||||
| HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | ||||
| Becker | Growth Inhibition Assay | IC50=75.1105 μM | ||||
| PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | ||||
| TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | ||||
| SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | ||||
| NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | ||||
| S-117 | Growth Inhibition Assay | IC50=75.755 μM | ||||
| HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | ||||
| CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | ||||
| BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | ||||
| LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | ||||
| LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | ||||
| ES8 | Growth Inhibition Assay | IC50=78.0073 μM | ||||
| UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | ||||
| NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | ||||
| IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | ||||
| BHY | Growth Inhibition Assay | IC50=79.596 μM | ||||
| MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | ||||
| IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | ||||
| WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | ||||
| VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | ||||
| NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | ||||
| MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | ||||
| 639-V | Growth Inhibition Assay | IC50=84.6129 μM | ||||
| RT4 | Growth Inhibition Assay | IC50=85.2403 μM | ||||
| NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | ||||
| CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | ||||
| BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | ||||
| HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | ||||
| G-361 | Growth Inhibition Assay | IC50=88.1474 μM | ||||
| LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | ||||
| HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | ||||
| DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | ||||
| CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | ||||
| MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | ||||
| HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | ||||
| SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | ||||
| NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | ||||
| SW872 | Growth Inhibition Assay | IC50=100.456 μM | ||||
| COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | ||||
| MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | ||||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
Chemische informatie, opslag en stabiliteit
| Molecuulgewicht | 390.41 | Formule | C19H21F3N6 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 1255517-76-0 | SDF downloaden | Opslag van stamoplossingen |
|
|
| Synoniemen | N/A | Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
Oplosbaarheid
|
In vitro |
DMSO
: 30 mg/mL
(76.84 mM)
Ethanol : 8 mg/mL Water : Insoluble |
Molariteitscalculator
|
In vivo |
|||||
In vivo formulatiecalculator (heldere oplossing)
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
Werkingsmechanisme
| Targets/IC50/Ki |
p70 S6K1
(Cell-free assay) 160 nM
|
|---|---|
| In vitro |
PF-4708671 is een piperazinyl-pyrimidine analoog en de eerste S6K1-specifieke remmer. Deze verbinding remt de activiteit van het nauw verwante S6K2-isoform of een aantal andere AGC-kinasen (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 of SGK1) niet significant. Het voorkomt de S6K1-gemedieerde fosforylering van S6-eiwit als reactie op IGF-1 (insuline-achtige groeifactor 1), terwijl het geen effect heeft op de PMA-geïnduceerde fosforylering van substraten van de sterk verwante RSK (p90 ribosomale S6 kinase) en MSK (mitogen- en stress-geactiveerde kinase) kinasen. Van deze chemische stof is ook gevonden dat het de fosforylering van de T-loop en het hydrofobe motief van S6K1 induceert, een effect dat afhankelijk is van mTORC1 (mTOR complex 1). Het beïnvloedt de activiteit van mTORC1 niet.
|
Referenties |
Toepassingen
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | p-mTOR / mTOR / p-p70S6K / p70S6K pS6 / S6 / pS6K / S6K1 / pAKT / AKT |
|
30423811 |
| Growth inhibition assay | Cell viability |
|
30423811 |
Technische ondersteuning
Tel: +1-832-582-8158 Ext:3
Als u nog andere vragen heeft, laat dan een bericht achter.
Veelgestelde vragen
Vraag 1:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for it is suitable for i.p. or not?
Antwoord:
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one for this compound. It is a suspension.
Producten zijn uitsluitend voor onderzoeksdoeleinden. Niet voor menselijk gebruik. Wij verkopen niet aan patiënten.
©Copyright 2013 Selleck Chemicals. Alle rechten voorbehouden.